1. Field of the Invention
The present invention is related to a non-steroidal analgesic anti-inflammatory adhesive preparation which contains as the pharmacologically effective component S-(+)-2-(2-fluoro-4-biphenylyl) propionic acid abbreviated S-(+)-FP hereinafter! which is optically resolved from the racemic modification 2-(2-fluoro-4-biphenylyl) propionic acid (also called: flurbiprofen).
2. Prior Art
Adhesive preparations, which can be broadly classified into poultices and plasters, are generally composed of a pharmacologically effective component, an adhesive which contains a plaster base as the principle components and further contains, as necessary, tackifiers, softeners, as well as solubilizing agents helpful in percutaneous absorption, and a flexible support which retains this adhesive in a layer shape. Then, a non-steroidal analgesic anti-inflammatory drug of one kind, or two or more kinds selected from methyl salicylate, glycol salicylate, emorfazone, diflunisal, oxaprozin, diclofenac, fenbufen, alclofenac, amfenac, indometacin, acemetacin, metiazinic acid, suprofen, ibuprofen, ketoprofen, flurbiprofen, fenoprofen, thiaprofen, tolmetin, naproxen, pranoprofen, protizinic acid, fentiazac, sulindac, clidanac, loxoprofen, lobenzarit, tolfenamic acid, flufenamic acid, and mefenamic acid, and their salts and esters etc. are normally used as the pharmacologically effective component of the non-steroidal analgesic anti-inflammatory adhesive preparation.
Not limited to non-steroidal analgesic anti-inflammatory adhesive preparations, the most important factor in all kinds of adhesive preparations is to be able to administer the pharmacologically effective component of adhesive preparation to the affected area percutaneously with good efficiency, and in order to realize this, several proposals were made in conventional technology.
For example, Japanese Patent Kokai No. 40,420/89 has the purpose of increasing the solubility of the non-steroidal analgesic anti-inflammatory drug into the plaster base, and also of increasing the percutaneous absorption. This patent indicated the use of styrene-isoprene-styrene block copolymers as the plaster base, polyterpene resin, terpene phenol resin or petroleum resin as the tackifier, liquid paraffin as the softener, and mentha oil as the solubilizing agent. Also, it is indicated in Japanese Patent Kokai No. 321,624/92 that, in order to improve the solubility of 4-biphenylacetic acid (also called: felbinac) which is one kind of analgesic anti-inflammatory drug, and of the ethyl esters thereof (also called: felbinac ethyl) into the plaster base, a styrene-isoprene-styrene block copolymer was selected for the plaster base, and this was used together with crotamiton.
In this regard, within all the kinds of non-steroidal analgesic anti-inflammatory drugs described above, flurbiprofen is synthesized as a racemic modification which a mixture of equal amount of dextrorotatory flurbiprofen and levorotatory flurbiprofen, and conventionally it was extremely difficult to resolve these racemic modifications. For this reason, if flurbiprofen is used as the non-steroidal analgesic anti-inflammatory drug, the precedent was to use these racemic modifications as is.
However, racemic flurbiprofen can be resolved into dextrorotatory flurbiprofen and levorotatory flurbidrofen by a method described in Patent Publication No. 6,536/87 entitled "Production Method for Optically Active 2-Aryl Propionic Acid."
One of the purposes of the present invention is to take advantage of the fact that dextrorotatory flurbiprofen has exceptionally superior efficacy as an analgesic anti-inflammatory drug for adhesive preparations than does racemic flurbiprofen, and offers a non-steroidal analgesic anti-inflammatory adhesive preparation which uses dextrorotatory flurbiprofen, namely, S-(+)-FP, as the pharmacologically effective component.
The other purpose of the present invention is to offer a plaster base which is suitable to the dissolution and dispersion of dextrorotatory flurbiprofen, a tackifier for this, as well as an assistant to promote the percutaneous absorption of dextrorotatory flurbiprofen.